An aryl <stereo>beta</stereo>-<stereo>D</stereo>-glucoside that is phloretin attached to a <stereo>beta</stereo>-<stereo>D</stereo>-glucopyranosyl residue at position 2' via a glycosidic linkage. ChEBICHEBI:8113

Phlorizin, a natural product and dietary constituent found in a number of fruit trees, is a 2'-glucoside of phloretin, Phlorizin is a competitive and classic inhibitor of hSGLT1(Ki=300 nM) and hSGLT2(
Ki= 39 nM). MedChem Expresshttp://www.medchemexpress.com/Orotic-acid.html, HY-N0143

Phlorizin, a natural product and dietary constituent found in a number of fruit trees, is a 2'-glucoside of phloretin, Phlorizin is a competitive and classic inhibitor of hSGLT1(Ki=300 nM) and hSGLT2(Ki= 39 nM). ;IC50 value: 300 nM (Ki, SGLT1); 39 nM (Ki, SGLT2) [1];Target: SGLT1; SGLT2;In vitro: Inhibition by phlorizin was competitive, with K(i) values of 0.3 muM in hSGLT1 and 39 nM in hSGLT2 [1]. Phlorizin was unable to exchange with dapagliflozin bound to hSGLT2. In contrast, dapagliflozin, fluoro-dapagliflozin, and galacto-dapagliflozin dissociated quickly from hSGLT1 (t(1/2,Off) = 1-2 s), and phlorizin readily exchanged with dapagliflozin bound to hSGLT1 [2].;In vivo: A PK-PD model was developed next to analyze the inhibitory effect of phlorizin on renal glucose reabsorption. The model suitably expressed the concentration-dependent inhibitory effect of phlorizin on renal glucose reabsorption. The in vivo inhibition constants of phlorizin for SGLT in rats were estimated to be MedChem ExpressHY-N0143